glutamate transporters

Chelidamic acid is a heterocyclic organic acid with a pyran skeleton and acts as an inhibitor of glutamate decarboxylase, with a Ki of 33 μM.

Troriluzole is an orally active glutamate modulator with anticancer activity.Troriluzole enhances the expression of excitatory amino acid transporters located in glial cells and is used in the study of spinocerebellar ataxia, Alzheimer's disease, and generalized anxiety disorder (GAD).

MS-153, identified as a compound that activates glutamate transporters, has been shown to reduce the conditioned reward effects of morphine, methamphetamine, and cocaine, without adversely affecting the acute locomotor response in mice.

Prasterone is an endogenous steroid hormone. Prasterone acts as an agonist at ERβ, NMDA, and σ1 receptors, a partial agonist at ERα and AR, and antagonist at GABA-A receptors. It displays a variety of biologocial activities, including enhancing working me

DL-TBOA ammonium is a potent, non-transportable inhibitor of excitatory amino acid transporters. Its inhibitory effects are demonstrated by IC50 values of 70 μM, 6 μM, and 6 μM for excitatory amino acid transporter-1 (EAAT1), EAAT2, and EAAT3, respectively. Additionally, DL-TBOA ammonium significantly hampers the uptake of [14C]glutamate in COS-1 cell lines expressing human EAAT1 and EAAT2, evident by Ki values of 42 μM and 5.7 μM, respectively. Furthermore, this compound competitively blocks EAAT4 and EAAT5, with Ki values of 4.4 μM and 3.2 μM, respectively.

(-)-Dizocilpine maleate ((-)-MK 801 (Maleate)) is a potent, selective, and non-competitive NMDA receptor antagonist, with a Kd of 37.2 nM in rat brain membranes.

YM 298198 Hydrochloride is a non-competitive antagonist with high affinity and selectivity for mGlu1 receptors (Ki = 19 nM). YM 298198 Hydrochloride is inactive at other mGlu receptor subtypes (mGlu2-7), ionotropic receptors and glutamate transporters (IC50 > 10 μM). It inhibits glutamate-induced IP production more potently than CPCCOEt (IC50 values are 16 nM and 6.3 μM respectively).